Diisopropylethylamine → 4,6-Dimethoxy-2-(alpha-fluorobenzyl) pyrimidine

HRID 1440962Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1440962
Cl.Cl.[C:3](=[NH:11])([O:9][CH3:10])[CH2:4][C:5](=[NH:8])[O:6][CH3:7].C(N(C(C)C)C(C)C)C.[F:21][CH:22]([C:26]1[CH:31]=[CH:30][CH:29]=[CH:28][CH:27]=1)[C:23](Cl)=O>ClCCl>[CH3:7][O:6][C:5]1[CH:4]=[C:3]([O:9][CH3:10])[N:11]=[C:23]([CH:22]([F:21])[C:26]2[CH:31]=[CH:30][CH:29]=[CH:28][CH:27]=2)[N:8]=1

Komponenten

5

Edukt 3

HCID 81531DiisopropylethylamineHCID 12896693Dimethyl malonimidate dihydrochlorideHCID 149495282-Fluoro-2-phenylacetyl chloride

Produkt 1

HCID 541012184,6-Dimethoxy-2-(alpha-fluorobenzyl) pyrimidineAusbeute 103,4 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel3×

Versuchsvorschrift

Dimethyl malonimidate dihydrochloride (11.0 g) was suspended in dichloromethane (100 ml) at -40° C. Ethyl diisopropylamine (38.9 ml) was added dropwise over 15 minutes at -40° C., followed by 2-fluoro-2-phenylacetyl chloride (11.0 g) in dichloromethane (15 ml) over 10 minutes at -40° C. The reaction mixture was allowed to warm to room temperature and stand overnight. It was then diluted further with dichloromethane, washed with ammonium chloride solution, then with water, and was dried over magnesium sulfate. The dichloromethane solution was evaporated to dryness to give 13.9 g of the desired product.

Aufarbeitung

  1. washwashed with ammonium chloride solution
  2. dry with materialwith water, and was dried over magnesium sulfate
  3. customThe dichloromethane solution was evaporated to dryness

Quellen und Nachweise

ORD-Eintrag
ord-6138cea4710c432493891253a750fc80
Quelldatensatz
uspto-grants-1996_03
Patentnummer
US05502028

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